Assay Detail
Binding
CHEMBL5519924
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 30 mins by TR-FRET assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Advancements in dual-target inhibitors of PI3K for tumor therapy: Clinical progress, development strategies, prospects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.31 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | 9.40 |
| CHEMBL5278435 | — | — | 1 | 9.34 |
| CHEMBL589258 | — | — | 1 | 8.85 |
| CHEMBL5426067 | — | — | 1 | 8.49 |
| CHEMBL1091978 | — | — | 1 | 8.40 |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 8.40 |
| CHEMBL3218578 | BGT-226 FREE BASE | 2.0 | 1 | 8.40 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | 8.30 |
| CHEMBL4297181 | SAMOTOLISIB | 2.0 | 1 | 8.22 |
| CHEMBL4071083 | — | — | 1 | 7.82 |
| CHEMBL4084907 | BIMIRALISIB | 2.0 | 1 | 7.48 |
| CHEMBL2322228 | — | — | 1 | 7.47 |
| CHEMBL3545366 | VOXTALISIB | 2.0 | 1 | 7.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL592445 | GEDATOLISIB | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5278435 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL589258 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5426067 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1091978 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3218578 | BGT-226 FREE BASE | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1922094 | APITOLISIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4297181 | SAMOTOLISIB | IC50 | = | 6.07 | nM | 8.22 |
| CHEMBL4071083 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4084907 | BIMIRALISIB | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2322228 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3545366 | VOXTALISIB | IC50 | = | 39.0 | nM | 7.41 |